1. Protein Tyrosine Kinase/RTK
  2. FAK
    Pyk2

PF-562271 besylate (Synonyms: PF562271 besylate; PF 562271 besylate)

Cat. No.: HY-10458 Purity: 98.31%
Handling Instructions

PF-562271 (besylate) is a potent, ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase with IC50 of 1.5 nM and 13 nM, and has > 100-fold selectivity against other protein kinases, except for some CDKs.

For research use only. We do not sell to patients.
PF-562271 besylate Chemical Structure

PF-562271 besylate Chemical Structure

CAS No. : 939791-38-5

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 123 In-stock
5 mg USD 84 In-stock
10 mg USD 108 In-stock
50 mg USD 300 In-stock
100 mg USD 540 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of PF-562271 besylate:

    PF-562271 besylate purchased from MCE. Usage Cited in: Int J Cancer. 2015 Oct 1;137(7):1549-59.

    786-O (a) and Caki-1 (b) are treated for 24 and 48h with increasing concentrations of PF-562,271 and adherent cells were counted. Cell lysates are evaluated through immunoblotting for total FAK following treatment for 24h.

    PF-562271 besylate purchased from MCE. Usage Cited in: Cancer Res. 2013 May 1;73(9):2873-83.

    FAK inhibition downregulates the AKT/mTOR pathway and CAS activity. A, protein levels measured by Western immunoblotting for AKT/mTOR pathway proteins in A673 and TC32 cells serum-starved overnight, treated with PF-562271 for 6 hours, and then stimulated with IGF-1 for 2 hours. Vinculin is used as the loading control. B, Western immunoblots showing downregulation of phospho-CAS but not phospho-ERK in A673 and TC32 cells after treatment with PF-562271.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    PF-562271 (besylate) is a potent, ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase with IC50 of 1.5 nM and 13 nM, and has > 100-fold selectivity against other protein kinases, except for some CDKs.

    IC50 & Target

    IC50: 1.5 nM (FAK), 13 nM (Pyk2)

    In Vitro

    PF-562,271 is a 30- to 120-nM (15.2 to 60.1 ng/mL) inhibitor of cdk2/E, cdk5/p35, cdk1/B, and cdk3/E in recombinant enzyme assays[1]. PF-562,271 blocks bFGF-stimulated blood vessel angiogenesis as performed in chicken chorioallantoic membrane assays[2]. Treatment of cells with PF-562,271 or knock-down of FAK by siRNA is observed to increase cell-cell adhesion strength[3].

    In Vivo

    PF-562,271 (33 mg/kg, p.o.) inhibits FAK phosphorylation in tumors in a dose- and time-dependent manner in tumor-bearing mice. FAK phosphorylation inhibition relative to total blood concentration of PF-562,271 results in a calculated EC50 of 93 ng/mL. PF-562,271 (25 mg/kg, p.o.) induces apoptosis 2-fold greater in treated tumors compared with vehicle-treated control tumors on day 3[1]. PF-562,271 (33 mg/kg, p.o.) and dasatinib extensively inhibit the movement of tumor cells in the animals. Inhibition of FAK kinase activity following treatment with PF-562,271 results in altered E-cadherin dynamics in vivo[3].

    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 1.5023 mL 7.5113 mL 15.0227 mL
    5 mM 0.3005 mL 1.5023 mL 3.0045 mL
    10 mM 0.1502 mL 0.7511 mL 1.5023 mL
    Please refer to the solubility information to select the appropriate solvent.
    Kinase Assay
    [1]

    Briefly, purified-activated FAK kinase domain (amino acid 410-689) is reacted with 50 μM ATP and 10 μg per well of a random peptide polymer of Glu and Tyr, p(Glu/Tyr), in kinase buffer [50 mM HEPES (pH 7.5), 125 mM NaCl, and 48 mM MgCl2] for 15 min. Phosphorylation of p(Glu/Tyr) is challenged with serially diluted compound at 1/2-Log concentrations starting at a top concentration of 1 μM. Each concentration is tested in triplicate. Phosphorylation of p(Glu/Tyr) is detected with a general antiphospho-tyrosine (PY20) antibody followed by horseradish peroxidase (HRP)-conjugated goat anti-mouse IgG antibody. HRP substrate is added, and absorbance readings at 450 nm are obtained after addition of stop solution (2mol/LH2SO4). IC50 values are determined using the Hill-Slope Model. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    PF-562271 is dissolved in 5% Gelucire.

    Exponentially growing cells are trypsinized and resuspended in sterile PBS and inoculated s.c. (1×106 cells per mouse in 200 μL) into the right flank of mice. Animals bearing tumors of appr 150 mm3 in size are divided into groups receiving either vehicle (5% Gelucire) or PF-562,271 (diluted in vehicle), and dosed by p.o. gavage. Animal body weight and tumor measurements are obtained every 2 d. Tumor volume (mm3) is measured with Vernier calipers and calculated. For all tumor growth inhibition experiments, 8 to 10 mice per dose group are used. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    665.66

    Formula

    C₂₇H₂₆F₃N₇O₆S₂

    CAS No.

    939791-38-5

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: 21.4 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Product Name:
    PF-562271 besylate
    Cat. No.:
    HY-10458
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